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Updated: Nov 15, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis of Some Novel Benzimidazole Derivatives as Anticancer Agent and Evaluation for CDK2 Inhibition Activity
Rania Helmy Abd El-Hameed1, Samar Said Fatahala1, Amira Ibrahim Sayed1
1Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo, Egypt.
Background:
Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules; they can easily interact with biomolecules of living systems.
Objective:
A series of substituted 2-thiobezimidazoles have been synthesized. Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell lines.
Methods:
The spectral data of the synthesized compounds were characterized. A docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib, were performed.
Results:
Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in the CDK-ATP binding pocket .3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib.
Conclusion:
Against all tested compounds; two compounds 3c &3l were found active against two types of cell-lines.
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